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1. 发明申请

WO1995030669A1 ETHER DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：其他衍生物和含有它们的药物组合物
公开(公告)号：WO1995030669A1
公开(公告)日：1995-11-16
申请号：PCT/GB1995001001
申请日：1995-05-02
申请人： ZENECA LIMITED , ZENECA-PHARMA , EDWARDS, Philip, Neil
发明人： ZENECA LIMITED , ZENECA-PHARMA
IPC分类号： C07D309/10
CPC分类号： C07D309/10
摘要： The invention concerns an ether derivative of formula (I), wherein each of A and A includes, independently, direct links; wherein X includes thio; wherein Ar includes phenylene, optionally substituted; wherein Ar includes phenylene, optionally substituted; wherein R and R independently includes hydrogen and (1-6C)alkyl; wherein R and R together, and R and R together, form a group of the formula -A -X -A -, which together with the carbon atom to which both A and A are attached define 4- to 7-membered rings, optionally substituted, wherein A and A are independently (1-4C)alkylene and X includes oxy; or wherein R and R together with the carbon atom to which both R and R are attached define cyclopentyl or cyclohexyl groups, optionally substituted; or a pharmaceutically-acceptable salt; and processes for their preparation, pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式（I）的醚衍生物，其中A 1和A 2各自独立地包括直链; 其中X 1包括硫代; 其中Ar 1包括任选取代的亚苯基; 其中Ar 2包括任选取代的亚苯基; 其中R 1和R 4独立地包括氢和（1-6C）烷基; 其中R 2和R 3一起并且R 5和R 6一起形成式-A 3 -X 2 -A 4 - 的基团，其与 A 3和A 4均连接的碳原子定义为任选取代的4-至7-元环，其中A 3和A 4独立地为（1-4C）亚烷基， 2>包括氧基; 或其中R 5和R 6与R 5和R 6两者所连接的碳原子一起定义为任选取代的环戊基或环己基; 或药学上可接受的盐; 及其制备方法，含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

2. 发明申请

WO1994029291A1 ANILINE DERIVATIVES 审中-公开
标题翻译：苯胺衍生物
公开(公告)号：WO1994029291A1
公开(公告)日：1994-12-22
申请号：PCT/EP1994001808
申请日：1994-06-03
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , EDWARDS, Philip, Neil
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D309/10
CPC分类号： C07D405/12 , C07D309/10
摘要： The invention concerns an aniline derivative of formula (I) wherein R includes hydrogen and (1-4C)alkyl; R includes hydrogen and (1-4C)alkyl; R is hydrogen or (1-4C)alkyl; X includes a group of the formula CR R wherein R is hydrogen or (1-4C)alkyl and R is hydrogen or (1-4C)alkyl; A includes a direct link to X ; X includes thio and sulphonyl; Ar includes phenylene, which may be optionally substituted; R includes hydrogen and (1-4C)alkyl; and R and R together form a ring having 5 to 6 ring atoms including one oxygen atom, and which ring may bear one, two or three substituents, including methyl alpha to the oxygen atom; or a pharmaceutically acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式（I）的苯胺衍生物，其中R 4包括氢和（1-4C）烷基; R 5包括氢和（1-4C）烷基; R 6是氢或（1-4C）烷基; X 3包括式CR 7 R 8的基团，其中R 7是氢或（1-4C）烷基，R 8是氢或（1-4C）烷基; A <1>包括与X <1>的直接链接; X 1包括硫代和磺酰基; Ar包括可以任选取代的亚苯基; R 1包括氢和（1-4C）烷基; 并且R 2和R 3一起形成具有5至6个环原子的环，包括一个氧原子，并且该环可以带有一个，两个或三个取代基，包括氧原子的甲基α; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

3. 发明申请

WO1994027999A1 BICYCLIC ETHER DERIVATIVES AND THEIR USE AS 5-LIPOXYGENASE INHIBITORS 审中-公开
标题翻译：双相醚衍生物及其作为5-LIPOXYGENASE抑制剂的用途
公开(公告)号：WO1994027999A1
公开(公告)日：1994-12-08
申请号：PCT/EP1994001805
申请日：1994-06-03
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , EDWARDS, Philip, Neil
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D493/08
CPC分类号： C07D495/08
摘要： The invention concerns a bicyclic ether derivative of formula (I), wherein Ar is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; A is a direct link to the group X or A is (1-4C)alkylene; X is oxy, thio, sulphinyl or sulphonyl; Ar is phenylene, pyridinediyl, pyrimidinediyl, thiophendiyl, furandiyl or thiazolediyl; and R is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式（I）的双环醚衍生物，其中Ar 1是苯基或萘基，或含有一个或两个氮杂原子并任选地含有另外选自氮，氧和硫的杂原子的10元双环杂环部分 ; A是直接连接到X基团或A是（1-4C）亚烷基; X是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基或噻唑二基; 并且R 1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

4. 发明申请

WO0049007A8 ACETAMIDO ACETONITRILE DERIVATIVES AS INHIBITORS OF CATHEPSIN L AND/OR CATHEPSIN S 审中-公开
标题翻译：作为CATHEPSIN L和/或CATHEPSIN S的抑制剂的乙酰胺乙酰胆碱衍生物
公开(公告)号：WO0049007A8
公开(公告)日：2001-03-15
申请号：PCT/GB0000532
申请日：2000-02-16
申请人： ASTRAZENECA AB , TUCKER HOWARD , LARGE MICHAEL STEWART , OLDFIELD JOHN , JOHNSTONE CRAIG , EDWARDS PHILIP NEIL
发明人： TUCKER HOWARD , LARGE MICHAEL STEWART , OLDFIELD JOHN , JOHNSTONE CRAIG , EDWARDS PHILIP NEIL
IPC分类号： A61K31/277 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4164 , A61K31/429 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/5377 , A61P3/14 , A61P11/00 , A61P43/00 , C07C255/29 , C07C311/13 , C07C311/19 , C07C323/52 , C07C323/60 , C07D207/327 , C07D213/57 , C07D231/18 , C07D233/84 , C07D307/38 , C07D307/54 , C07D333/24 , C07D409/04 , C07D409/12 , C07D417/04 , C07D513/04 , A61K31/275 , A61K31/335 , A61K31/38
CPC分类号： C07D409/04 , C07C255/29 , C07D213/57 , C07D231/18 , C07D233/84 , C07D307/54 , C07D333/24 , C07D409/12 , C07D513/04
摘要： A compound of formula (I) wherein Ar, R , R , R , R and R are defined; a composition comprising a compound of formula (I) and a carrier or diluent; a compound of formula (I) for use as a medicament, the use of a compound of formula (I) in the manufacture of a medicament for use in the inhibition of a cysteine protease in a warn blooded animal; the use of a compound of formula (I) in the manufacture of a medicament for use in the treatment of chronic obstructive pulmonary disease in a warm blooded animal; and a method of treating a Cathepsin L or Cathepsin S mediated disease state in mammals which comprises administering to a mammal in need of such treatment an effective amount of a compound of formula (I).
摘要翻译：定义其中Ar，R 1，R 2，R 3，R 4和R 5的式（I）化合物; 包含式（I）化合物和载体或稀释剂的组合物; 用于药物的式（I）化合物，式（I）化合物在制备用于抑制警戒血液动物中的半胱氨酸蛋白酶的药物中的用途; 式（I）化合物在制备用于治疗温血动物慢性阻塞性肺疾病的药物中的用途; 以及治疗哺乳动物中组织蛋白酶L或组织蛋白酶S介导的疾病状态的方法，其包括向需要这种治疗的哺乳动物施用有效量的式（I）化合物。

5. 发明申请

WO9921860B1 PHENANTHROLINE DERIVATIVES 审中-公开
标题翻译：苯并噻吩衍生物
公开(公告)号：WO9921860B1
公开(公告)日：1999-08-05
申请号：PCT/US9822704
申请日：1998-10-26
申请人： FIBROGEN INC , ZENECA LTD , EDWARDS PHILIP NEIL , LARGE MICHAEL STEWART , HALES NEIL JAMES , MARTIN GEORGE R , HUANG XINFAN
发明人： EDWARDS PHILIP NEIL , LARGE MICHAEL STEWART , HALES NEIL JAMES , MARTIN GEORGE R , HUANG XINFAN
IPC分类号： A61K31/4745 , A61K31/496 , A61K31/5377 , A61P1/16 , A61P17/02 , A61P19/02 , A61P29/00 , A61P43/00 , C07D471/04 , A61K31/47
CPC分类号： C07D471/04 , A61K31/4745
摘要： The present invention provides a phenanthroline derivative of formula (I) wherein, for example, R is hydrogen, carboxy, cyano, nitro, (1-4C)alkyl, (1-6C)alkoxycarbonyl, (1-4C)alkylamino, (2-4C)alkanoyl, (1-4C)alkoxy-(2-4C)alkoxy-(2-4C)alkoxycarbonyl or N -[amino-(2-8C)alkyl]carbamoyl; R is, for example, hydrogen, carboxy, (1-6C)alkoxycarbonyl, carbamoyl, N -(1-8C)alkylcarbamoyl, N , N -di-(1-8C)alkylcarbamoyl, N -(1-4C)alkylcyclohexylcarbamoyl, 1,2,3,4,-tetrahydro-isoquinolin-2-ylcarbonyl or N , N -[di-(1-4C)alkyl]thiocarbamoyl; R and R , which may be the same or different, are, for example, hydrogen or halo; and R is, for example, hydrogen, di-(1-4C)alkylamino or halo; or a pharmaceutically-acceptable salt thereof. The invention further provides pharmaceutical compositions comprising phenanthroline derivatives, processes for making the same and their use in producing an anti-fibroproliferative effect.
摘要翻译：本发明提供式（I）的菲咯啉衍生物，其中例如R 1是氢，羧基，氰基，硝基，（1-4C）烷基，（1-6C）烷氧基羰基，（1-4C）烷基氨基，（2-4C）烷酰基，（1-4C）烷氧基 - （2-4C）烷氧基 - （2-4C）烷氧基羰基或N - [氨基 - （2-8C）烷基]氨基甲酰基; R 2是例如氢，羧基，（1-6C）烷氧基羰基，氨基甲酰基，N - （1-8C）烷基氨基甲酰基，N， N 1 - （1-8C）烷基氨基甲酰基，N - （1-4C）烷基环己基氨基甲酰基，1,2,3,4 - 四氢 - 异喹啉-2-基羰基或ñ，ñ - [二 - （1-4C）烷基]硫代氨基甲酰基; R 3和R 4可以相同或不同，例如是氢或卤素; 和R 5是例如氢，二 - （1-4C）烷基氨基或卤素; 或其药学上可接受的盐。本发明还提供了包含菲咯啉衍生物的药物组合物，其制备方法及其在产生抗纤维增生作用中的用途。

6. 发明申请

WO1997031023A1 PEPTIDE DERIVATIVES 审中-公开
标题翻译：肽衍生物
公开(公告)号：WO1997031023A1
公开(公告)日：1997-08-28
申请号：PCT/GB1997000438
申请日：1997-02-18
申请人： ZENECA LIMITED , COTTON, Ronald , EDWARDS, Philip, Neil , LUKE, Richard, William, Arthur
发明人： ZENECA LIMITED
IPC分类号： C07K14/725
CPC分类号： C07K14/4713 , A61K38/00 , C07K14/70539
摘要： The invention concerns pharmaceutically useful peptide derivatives of the formula (I): P-R -R -R -R , in which P, R , R , R , and R have the various meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel peptide derivatives are of value in treating MHC class II dependent T-cell mediated autoimmune or inflammatory diseases, such as rheumatoid arthritis. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds in medical treatment.
摘要翻译：本发明涉及式（I）的药学上有用的肽衍生物：其中P，R 1，R 2，R 2，R 3， 3＆gt;和R 4具有本文定义的各种含义及其药学上可接受的盐和含有它们的药物组合物。新型肽衍生物在治疗MHC II类依赖性T细胞介导的自身免疫性或炎性疾病如类风湿性关节炎中是有价值的。本发明还涉及制备新型肽衍生物的方法和该化合物在医疗中的用途。

7. 发明申请

WO1996023749A1 CHEMICAL LIBRARIES, LABELLING AND DECONVOLUTION THEREOF 审中-公开
标题翻译：化学图书馆，标签和解体
公开(公告)号：WO1996023749A1
公开(公告)日：1996-08-08
申请号：PCT/GB1996000197
申请日：1996-01-30
申请人： ZENECA LIMITED , EDWARDS, Philip, Neil , MAIN, Brian, Geoffrey , SHUTE, Richard, Eden
发明人： ZENECA LIMITED
IPC分类号： C07B61/00
CPC分类号： C40B40/04 , B01J2219/00459 , B01J2219/005 , B01J2219/00572 , B01J2219/00581 , B01J2219/00585 , B01J2219/00592 , B01J2219/00596 , B01J2219/0072 , C07B2200/11 , C08F8/00 , C08F8/14 , C08F8/18 , C08F8/26 , C40B20/04 , C40B50/16 , C08F112/14
摘要： A method for the preparation of a labelled chemical library which method comprises synthesizing the library on a plurality of solid supports each of which is provided with at least one inert label which label remains attached to the solid phase and is unaffected by library synthesis, so as to provide a chemical library comprising a plurality of solid supports to each of which is attached at least one inert label and at least one member of the chemical library.
摘要翻译：一种制备标记化学文库的方法，该方法包括在多个固体支持物上合成该文库，每个固体载体上均装有至少一个惰性标签，该标签保持附着在固相上，不受文库合成的影响，因此以提供包含多个固体支持物的化学文库，其中每个固体载体连接至少一个惰性标签和化学文库的至少一个成员。

8. 发明申请

WO1995030668A1 CYCLIC ETHER DERIVATIVES AND PHARMACEUTICAL COMPOSITION CONTAINING THEM 审中-公开
标题翻译：循环醚衍生物和含有它们的药物组合物
公开(公告)号：WO1995030668A1
公开(公告)日：1995-11-16
申请号：PCT/GB1995001000
申请日：1995-05-02
申请人： ZENECA LIMITED , ZENECA-PHARMA , EDWARDS, Philip, Neil , WATERSON, David
发明人： ZENECA LIMITED , ZENECA-PHARMA
IPC分类号： C07D309/06
CPC分类号： C07D405/12 , C07D309/06 , C07D413/12
摘要： The invention concerns a cyclic ether derivative of formula (I), wherein Ar is phenyl or naphthyl, or a 9- or 10-membered bicyclic heterocyclic moiety, and Ar may be optionally substituted; A includes (1-4C)alkylene; X includes oxy; Ar includes phenylene, pyridinediyl and pyrimidinediyl which may optionally bear one or two substituents; R and R together form a group of the formula: -A -X -A - which, together with the carbon atom to which both A and A are attached, define a 5- or 6-membered ring wherein: A is (1-3C)alkylene; X includes oxy; and A is (1-3C)alkylene; and which ring may be optionally substituted; and Y includes halogeno, 2-cyanovinyl, 2-halogenovinyl, hydroxyimino-(1-4C)alkyl and (1-4C)alkoxyimino-(1-4C)alkyl; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式（I）的环醚衍生物，其中Ar 1是苯基或萘基，或9或10元双环杂环部分，Ar 1可以任选被取代; A 1包括（1-4C）亚烷基; X 1包括氧基; Ar 2包括可以任选地带有一个或两个取代基的亚苯基，吡啶二基和嘧啶二基; R 1和R 2一起形成下式的基团：-A 2 -X 2 -A 3，其与A 2和A“ 3>连接，定义5-或6-元环，其中：A 2是（1-3C）亚烷基; X 2包括氧基; 并且A 3为（1-3C）亚烷基; 并且哪个环可以任选被取代; 和Y包括卤代，2-氰基乙烯基，2-卤代乙烯基，羟基亚氨基 - （1-4C）烷基和（1-4C）烷氧基亚氨基 - （1-4C）烷基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

9. 发明申请

WO2006123145A1 ANTIFUNGAL AGENTS 审中-公开
标题翻译：反真菌药
公开(公告)号：WO2006123145A1
公开(公告)日：2006-11-23
申请号：PCT/GB2006/001820
申请日：2006-05-18
申请人： F2G LTD , THOMSON, Samantha, Patricia , DAVIES, Rhian, Teresa , ALLANSON, Nigel, Mark , KUVSHINOV, Alexandre , DAVIES, Gareth, Morse , EDWARDS, Philip, Neil
发明人： THOMSON, Samantha, Patricia , DAVIES, Rhian, Teresa , ALLANSON, Nigel, Mark , KUVSHINOV, Alexandre , DAVIES, Gareth, Morse , EDWARDS, Philip, Neil
IPC分类号： A61K31/437 , A61P31/12
CPC分类号： A61K31/437
摘要： Compounds of formula (I), and pharmaceutically acceptable salts thereof, may be used in therapy, for example as antifungal agents: (I) wherein: Rl, R2, R3, R4, R5, R6, R7, X and X 1 are as defined herein. Certain compounds of formula (I) are also provided. Compounds of formula (T), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
摘要翻译：式（I）化合物及其药学上可接受的盐可用于治疗，例如抗真菌剂：（I）其中：R1，R2，R3，R4，R5，R6，R7，X和X 1 如本文所定义。还提供某些式（I）化合物。式（T）化合物及其农业上可接受的盐也可用作农业杀真菌剂。

10. 发明申请

WO1997046578A1 PEPTIDE DERIVATIVES 审中-公开
标题翻译：肽衍生物
公开(公告)号：WO1997046578A1
公开(公告)日：1997-12-11
申请号：PCT/GB1997001491
申请日：1997-06-03
申请人： ZENECA LIMITED , COTTON, Ronald , EDWARDS, Philip, Neil , LUKE, Richard, William, Arthur , OLDHAM, Keith
发明人： ZENECA LIMITED
IPC分类号： C07K07/02
CPC分类号： C07K7/06 , A61K38/00 , C07K7/02 , C07K14/4713 , Y10S530/825 , Y10S530/851
摘要： The invention concerns pharmaceutically useful peptide derivatives of the formula (I), P-AA -AA -AA -AA -AA -AA -AA -AA -Q, in which P, AA , AA , AA , AA , AA , AA , AA , AA , and Q have the various meanings defined herein and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel peptide derivatives are of value in treating MHC class II dependent T-cell mediated autoimmune or inflammatory diseases, such as rheumatoid arthritis. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds in medical treatment.
摘要翻译：本发明涉及式（I）的药学上可用的肽衍生物，P-AA 1 -AA 2 -AA 3 -AA 4 -AA 5 -AA 6 -AA 7 -A A 8 -A，其中P，AA 1，AA 2，AA 3，AA 4，AA 5，AA 6，AA 7，AA 8 >和Q具有本文定义的各种含义及其药学上可接受的盐，以及含有它们的药物组合物。新型肽衍生物在治疗MHC II类依赖性T细胞介导的自身免疫性或炎性疾病如类风湿性关节炎中是有价值的。本发明还涉及制备新型肽衍生物的方法和该化合物在医疗中的用途。

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